Vafidemstat (ORY-2001) is an oral, brain penetrant drug that inhibits LSD1 and MAOB by reducing cognitive impairment, including memory loss and neuroinflammation. It also has neuroprotective effects.

Disodium (R)-2-Hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 0.628 mM.

CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

TACH101 (QC8222, TACH 101) is a reversible, α-ketoglutarate competitive, selective and potent inhibitor of KDM4 isoforms A-D with IC50 values of <0.1 uM against all four isoforms.TACH101 demonstrated potent increase of H3K36me3 levels (EC50 <0.001 uM, HTRF) in KYSE-150 cell line engineered to overexpress KDM4C and showed potent anti-proliferative activity in multiple cell lines in OncoPanel.Sub-micromolar levels of TACH101 induced apoptosis in human colorectal (HT-29), esophageal (KYSE-150), and triple negative breast cancer (MDA-MB-231) cell lines with EC50s of 0.033-0.092 uM.TACH101 triggered effective tumor growth control in xenograft models including colorectal, esophageal, gastric, breast, and lymphoma with tumor growth inhibition of up to 100%.

ZY0511 is a highly selective and potent inhibitor of lysine-specific histone demethylase 1 (LSD1) with IC50 of 1.7 nM and SPR Kd of 2.42 nM.

WS-384 is a specific, small-molecule inhibitor dually targeting LSD1 (IC50=338.8 nM) and the DCN1-UBC12 interaction (IC50=14.8 uM).

iPHF8 (inhibitor of PHF8) is a specific inhibitor of protein demethylase PHF8 with IC50 of 2.01 uM in Succinate-Glo JmjC demethylase assays, and SPR KD value of 240 nM.

FTO-43 (FTO-43 N) is a potent, selective inhibitor of the m6A demethylase fat mass- and obesity-associated protein (FTO) with IC50 of 1.0 uM, no significant acitivity against the homologous m6A RNA demethylase ALKBH5 (IC50>40 uM).

EPZ020809 is a potent, specific KDM4C inhibitor with Ki of 31 nM, binds KDM4C in a 2-OG-competitive fashion.

CBA-1 is a small molecule inhibitor of Wnt signaling, specifically targets Jumonji (JmjC) domain-containing demethylase KDM3A with IC50 of 3.9 uM.

MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells.

Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity.

Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.

JADA82 (PCK82) is a potent KDM5A (lysine demethylase 5A) inhibitor. From patent WO2020033377A1.

ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases.

Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma.

SD49-7 is an inhibitor of histone lysine-specific demethylase 4 (KDM4) with an IC50 of 0.19 µM.

iJMJD6(WL12) is an inhibitor of arginine demethylase JMJD6 with an IC50 value of 0.22 μM.

CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. CPI-4203 is competitive with 2-oxoglutarate (2-OG). CPI-4203 is structurally related to CPI-455 but is less potent.

Zavondemstat is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity.

INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 dihydrochloride can be used for the research of myeloid leukemia.

SP2509 is a novel histone demethylase LSD1 (KDM1A) antagonist with IC50 of 13 nM; no inhibition on MAO-A and MAO-B.

Seclidemstat(SP-2577) is a potent LSD1 inhibitor, with a mean IC50 of 127 nM.

RN-1 is an inhibitor of lysine specific demethylase 1 (LSD1); exhibits selectivity for LSD1 over monoamine oxidase (MAO)-A and MAO-B (IC50 values are 70 nM, 0.51 and 2.79 μM respectively.

OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.

ML-324 is a JMJD2 histone demethylase inhibitor (JMJD2 IC50 = 920 nM)

IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.

GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 94 nM instead of 8.4 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells.

Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.